52 results about "Anticarcinogenic Agents" patented technology

The present invention relates to novel antibodies capable of binding specifically to the human insulin-like growth factor I receptor IGF-IR and / or capable of specifically inhibiting the tyrosine kinase activity of said IGF-IR receptor, especially monoclonal antibodies of murine, chimeric and humanized origin, as well as the amino acid and nucleic acid sequences coding for these antibodies. The invention likewise comprises the use of these antibodies as a medicament for the prophylactic and / or therapeutic treatment of cancers overexpressing IGF-IR or any pathology connected with the overexpression of said receptor as well as in processes or kits for diagnosis of illnesses connected with the overexpression of the IGF-IR receptor. The invention finally comprises products and / or compositions comprising such antibodies in combination with anti-EGFR antibodies and / or compounds and / or anti-cancer agents or agents conjugated with toxins and their use for the prevention and / or the treatment of certain cancers.

The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and / or Factor VIIa (FVIIa), and have utility as anti cancer agents and / or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.

The invention provides small molecule mimics of the Smac peptide that are dimer-like or trimer-like compounds having two or three amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.

Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunsupression associated with an infectious disease, e.g., HIV-1 infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.

The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and / or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.

The present invention concerns fragments and variants of the HYD1 peptide; polynucleotides encoding the peptides; host cells genetically modified with the polynucleotides; vectors comprising the polynucleotides; compositions containing these peptides, polynucleotides, vectors, or host cells; and methods of using the peptides, polynucleotides, vectors, and host cells as inhibitors of aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as myeloma. The present invention further includes a method of increasing the efficacy of chemotherapy and radiation therapy, comprising administering an agent that binds β1 integrin to a patient in need thereof. In one embodiment, the β1 integrin binding agent is the HYD1 peptide, or a functional fragment or variant thereof. In another aspect, the invention pertains to a composition (an adhesion trap) comprising a substrate (also referred to as a surface or support) with a HYD1 peptide, or fragment or variant thereof, immobilized to the substrate, and a method of removing circulating tumor cells (CTC) from blood by contacting a subject's blood with the immobilized peptide. Another aspect of the invention concerns a method of identifying modulators of peptide binding. Another aspect of the invention concerns a method for detecting CTC.

This invention is a method and kit for preparing a Tumor in Dish model for use in screening anti-cancer agents and analyzing cancer growth and development.

Disclosed are a diagnosis method and a therapeutic method for cancer, both of which utilize HERV-H env gene and protein. Particularly, cancer can be diagnosed by detecting the expression of HERV-H env gene, and a reagent used for the detection of the expression can be used as a diagnosing agent. Cancer can be treated by inhibiting the function of HERV-H env gene, and a reagent used for the inhibition of the function can be used as an anti-cancer agent. Alternatively, cancer can be treated by administering a peptide having a specific sequence contained in HERV-H env protein or the like, and the peptide or the like can be used as a cancer vaccine.

Compounds of formula (I): A-B-C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is formula (ii) RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1 , 2, or 3 of RA2 to RA6 are not H; C is formula (iii) where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and an optionally substituted N-containing C5-7 heterocyclic group; RC5 is a group selected from formula (iv) which group may be selected by one or two C1-4 alkyl groups or a carboxy group; RC6 is H; or, when X and Y are N, RC5 and RC6 (when Z is CRC6) together with the carbon atoms to which they are attached may form a fused C6 aromatic ring selected from the group consisting of formula (v).

A microfluidic device for more accurately modeling the in vitro environment in which cancer occurs is disclosed. The device comprises a surface defining one or more microfluidic channels that may further comprise one or more endothelial cells, a first three dimensional scaffold comprising one or more cancer cells that is spatially separated from the one or more microfluidic channels, and a second three dimensional scaffold comprising one or more stromal cells, at least a portion of which is interposed between the one or more microfluidic channels and the first three dimensional scaffold. The second three dimensional scaffold is in fluid communication with both the first three dimensional scaffold and the one or more microfluidic channels. The device can be used to assay anti-cancer agents, or as a system for modeling the growth, behavior, or metastasis and tumor formation of cancer cells.

The present invention relates to a process for preparation of crystalline Form-SDI of Dasatinib (I).Said crystalline Form-SDI of Dasatinib is characterized by X-ray powder diffraction pattern comprising of at least seven 2θ° peaks selected from the XRPD peak set of 5.8, 11.5, 12.7, 13.2, 17.3, 17.5, 18.1, 20.1, 20.5, 22.1, 25.4, 26.6, 26.8±0.20 2θ°; IR spectrum having at least five absorption peaks selected from about 3390 cm−1, 2923 cm−1, 1621 cm−1, 1615 cm−1, 1537 cm−1, 1316 cm−1, 1061 cm−1, 815 cm−1 and 783 cm−1; and DSC isotherm comprising at least two endothermic peaks ranging between −130° C. to 150° C., 160° C. to 175° C. or 280° C. to 290° C.The pharmaceutical compositions of the crystalline Form-SDI of Dasatinib or its hydrate thereof may be useful as an anti-cancer agent.

A pharmacologic agent for treating and / or preventing cancer, among other diseases and conditions, and particularly breast, prostate, and pancreatic cancer, in humans and animals. The novel pharmacologic agent is an isoflavonoid or isoflavonoid mimetic covalently attached to a cytotoxic pharmacophore that, preferably has the ability to conjugate with a metal salt to form a more potent metal complex, particularly a Cu(II) complex. The isoflavonoid or isoflavonoid mimetic may be non-fragmented steroidal hormone, such as progesterone which is structurally related to the isoflavone genistein, or a small molecule hormone mimetic, such as chromone. An illustrative non-fragmented steroidal embodiment is 17-acetyl-10,13-dimethyl-1,2,6,7,8,9,11,12,13,14,15,16,17-tetradecahydrocyclopenta[a]phenantnren-3-thiosemicarbazone and its Cu(II) complex. Effective chromone analogs include the thiosemicarbazone and hydrazone analogs of 4-oxo-4H-chromene-3-carboxaldehyde and their Cu(II) complexes.

The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I:and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.

The present invention relates to a method of defining the differentiation grade of tumor by selecting genes and / or proteins whose expression level correlates with each differentiation grade of tumor, measuring the expression of the genes and / or proteins of human tumor tissues in each differentiation grade. The present invention also relates to the use of these genes and / or proteins for diagnosing the differentiation grade of tumor and for screening anti-cancer agents for tumor treatment.

The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I:and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.

This invention provides a compound that is 4,4′-(4′-Carboxy)-4-nonyloxy-[1,1′-biphenyl]-3,5-diyl)dibutanoic acid (CNBDA), derivative compounds of CNBDA, and pharmaceutical compositions thereof. The derivative compounds of CNBDA have one or more of the following substitutions (a) replacement of one or both of the carboxylic acid groups of the CNBDA compound with an organic acid group having 1-3, or 5-30, or more carbon atoms in chain length, wherein the carbon atom chains are either saturated, partially saturated, or unsaturated with respect to the carbon to carbon bonding, (b) replacement of the carboxylic groups of (a) with a phosphate, a sulphate, an amide, a hydroxyl, an aldehyde, or a halide group, and (c) replacement of the nonane group with an alkane having a carbon chain length of 1-8 or 10-30, or more carbon atoms. A method of treating a patient having cancer is provided.

Disclosed are identified and successfully targeted microRNAs (miRNAs) associated with human cancer cell line response to a range of anti-cancer agents. The strategy of integrating in vitro miRNA expression and drug sensitivity data not only aid in the characterization of determinants of cytotoxic response, but also in the identification of novel therapeutic targets.

This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.

The invention provides a nucleic acid construct comprising a promoter sequence derived from microRNA-21 (miR-21) linked to a nucleic acid sequence encoding an anti-cancer agent, an example of which is a toxin. The constructs of the invention are particularly useful for treating tumors expressing miR-21.

The present invention provides a site-specific pegylated arginase conjugate and method for producing thereof. The site-specific pegylated arginase is homogeneous in molecular weight and shows therapeutic effect for treating cancers and viral infections. The method for producing the arginase conjugate comprises genetically modifying the gene encoding an arginase so that the PEG moiety can be attached to the enzyme at a predetermined, specific intended sites. This is achieved by removing the PEG-attaching amino acid residue(s) at undesirable site(s) while keeping or adding cysteine(s) at the desirable site(s) of the enzyme. Two exemplary embodiments of the pegylated arginase conjugate are directed to human arginase I (HAI) where a polyethylene glycol (PEG) moiety is site-specific covalently bonded to Cys45 of the enzyme and Bacillus caldovelox arginase (BCA) where a polyethylene glycol (PEG) moiety is site-specific covalently bonded to Cys161 of the enzyme.

The present invention relates to a method of defining the differentiation grade of tumor by selecting genes and / or proteins whose expression level correlates with each differentiation grade of tumor, measuring the expression of the genes and / or proteins of human tumor tissues in each differentiation grade. The present invention also relates to the use of these genes and / or proteins for diagnosing the differentiation grade of tumor and for screening anti-cancer agents for tumor treatment.

The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.

Described herein are self-assembling protein molecules for delivering a payload, for example, a toxic anti-cancer agent, a cancer immunotherapy, a toxic anti-cancer agent and a cancer immunotherapy, or an imaging agent, to specific tissues. Examples of self-assembled proteins include clathrin and derivatives of clathrin.

In one embodiment, the invention provides methods of treating or preventing cancer, in particular aspects breast and / or prostate cancer, by administering to a subject in need thereof a therapeutically-effective amount of irisin and, optionally, one or more adjuvant therapies (e.g. synergistic co-administration of an additional anti-cancer agent or chemotherapy). Related pharmaceutical compositions, assays and kits are also provided.

The present disclosure relates to compound of structural Formula I and a method for preparing said compounds. The disclosure further relates to a method of employing the Formula I compounds for modulation of Janus kinase-Signal Transducer and Activator of Transcription (JAK-STAT) pathway in cancer cells, and the corresponding use of compound of Formula I as anti-cancer agents.

The invention concerns compounds DLBS1425E2.2 and DLBS1425F1 isolated and identified from the extract of the plant Phaleria macrocarpa (Scheff.) Boerl. The invention also relates to the use of said compounds, either as a single active compound or in combination, in a pharmaceutical dosage form that has anti-proliferative activity of cancer cells, and its use relating to female related diseases. Formula (I).

The present disclosure relates to novel compounds that can be used as anti-cancer agents in the prostate cancer therapy. In particular, the invention relates to N-acyl derivatives of 2,3-dihydro-1H-pyrrolo[2,3-b]quinolines having the structural Formula (I),stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or pharmaceutically acceptable salt and / or solvate thereof. The meaning of R1 is independently selected from H; C1-C6 Alkyl, cyclo-Alkyl or iso-Alkyl substituents; R2 is selected from C1-C6 Alkyl, cyclo-Alkyl or iso-Alkyl; substituted or non-substituted, fused or non-fused to substituted or non-substituted aromatic ring, aryl or heteroaryl groups. The invention also relates to methods for preparing said compounds, and to pharmaceutical compositions comprising said compounds.

The present invention relates to novel benzylideneacetone derivatives or uses thereof, more specifically, the present invention relates to a pharmaceutical composition for preventing or treating, or food composition for ameliorating a cancer or a bone disease comprising a compound defined by Formula 1 or pharmaceutically acceptable salt thereof as an active ingredient.Since compounds according to the present invention exhibit strong inhibitory activity on proliferation and differentiation of osteoclast, and activity on proliferation and differentiation of osteoblast, it can be usefully used to develop safe and effective anti-cancer agents, and therapeutic agents for preventing and treating or foods for ameliorating bone diseases including osteoporosis, and the like.

Disclosed are nanoparticles comprising: an active compound, or a pharmaceutically acceptable salt or prodrug thereof, the active compound comprising a nucleobase analog moiety covalently linked to an omega-3 polyunsaturated fatty acid moiety; a pegylated vitamin E compound; and at least one oil phase component. Also disclosed are methods for treating a subject having a disease comprising administering to the subject a therapeutically effective amount of the disclosed nanoparticles. The compositions and methods are useful for the treatment of diseases, such as tumors, by delivering a range of active compounds, including, for example, 4-(N)-docosahexaenoyl 2 ', 2'-difluorodeoxycytidine (DHA-dFdC) or other hydrophobic and / or lipophilic anti-cancer agents. The compositions and methods are further useful for delivering pharmaceutical agents and / or nutritional agents via a variety of routes of administration. Methods of making the nanoparticles are also disclosed.

A majority of neuroendocrine (NE) cancers overexpress somatostatin receptors (SSTRs). Disclosed herein are anti-SSTR2 monoclonal antibodies, and antibody-drug conjugates (ADCs) for use as NE cancer targeting therapeutics. Also disclosed is an isolated nucleic acid encoding the disclosed antibodies, as well as nucleic acid vectors containing this isolated nucleic acid operably linked to an expression control sequence. Also disclosed are cells transfected with these vectors and the use of these cells to produce the disclosed recombinant antibodies. Also disclosed is a method of treating a neuroendocrine (NE) cancer in a subject, comprising administering to the subject an effective amount of the disclosed antibody conjugated to an anti-cancer agent.